Antiproliferative effects of JQ-EZ-05 on VHL−/− ccRCC are on-target

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Fig. 5. Antiproliferative effects of JQ-EZ-05 on VHL−/− ccRCC are on-target. Antiproliferative effects of JQ-EZ-05 on VHL−/− ccRCC are on-target. (A) Sequence alignment of EZH1 and EZH2 catalytic SET domains. (B and C) Immunoblots (B) and crystal violet staining (C) of 786-O cells infected to exogenously produce WT or ΔPSET EZH1 and treated with the indicated amounts of JQ-EZ-05 for 3 and 7 days, respectively. (D and E) Photomicrographs (D) and immunoblots (E) of 786-O cells infected with a lentivirus encoding GFP, WT EZH1, or randomly mutagenized EZH1 (XL-Red) and treated with the indicated concentrations of JQ-EZ-05 for 3 days (E) or with either 4 μM JQ-EZ-05 or DMSO for 21 days (D). (F) Crystal violet staining of UMRC-2 cells infected to exogenously produce the indicated EZH1 variants and treated with the indicated concentrations of JQ-EZ-05 for 10 days. (G) Structural model of JQ-EZ-05 bound to WT EZH1. (H) Immunoblots of UMRC-2 cells expressing EZH1 variants as in (F) treated with the indicated concentrations of JQ-EZ-05 for 3 days. Abhishek A. Chakraborty et al., Sci Transl Med 2017;9:eaal5272 Published by AAAS